Assay Detail
Binding
CHEMBL646639
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Displacement of [125I]AB-MECA from adenosine A3 receptor from HEK293 cell membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.12 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.48 |
| CHEMBL119709 | IB-MECA | — | 1 | 8.96 |
| CHEMBL133566 | — | — | 1 | 8.82 |
| CHEMBL265096 | — | — | 1 | 8.57 |
| CHEMBL2112485 | — | — | 1 | 7.65 |
| CHEMBL2112486 | — | — | 1 | 7.56 |
| CHEMBL2112484 | — | — | 1 | 7.30 |
| CHEMBL2112483 | — | — | 1 | 6.64 |
| CHEMBL107155 | — | — | 1 | 5.68 |
| CHEMBL105764 | — | — | 1 | 5.64 |
| CHEMBL107987 | — | — | 1 | 5.55 |
| CHEMBL108753 | — | — | 1 | 5.55 |
| CHEMBL100071 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL119709 | IB-MECA | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL133566 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL265096 | — | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL2112485 | — | Ki | = | 22.5 | nM | 7.65 |
| CHEMBL2112486 | — | Ki | = | 27.7 | nM | 7.56 |
| CHEMBL2112484 | — | Ki | = | 50.5 | nM | 7.30 |
| CHEMBL2112483 | — | Ki | = | 229.0 | nM | 6.64 |
| CHEMBL107155 | — | Ki | = | 2110.0 | nM | 5.68 |
| CHEMBL105764 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL107987 | — | Ki | = | 2830.0 | nM | 5.55 |
| CHEMBL108753 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL100071 | — | Ki | = | 7240.0 | nM | 5.14 |